title: NF-κB inhibitory activity of sucrose fatty acid esters and related constituents from Astragalus membranaceus.
abstract: Twelve compounds, including six sucrose fatty acid esters (1-6), four galactosyl acylglycerols (7-10), and two sphingolipids (11 and 12), were isolated from the roots of Astragalus membranaceus . Their structures were identified on the basis of spectroscopic analysis. Among the isolated sucrose fatty acid esters, 6'-O-linoleyl sucrose (1) was identified as a new compound, and 6'-O-palmitoyl sucrose (2) and 6-O-palmitoyl sucrose (3) were isolated from nature for the first time. This is the first report on sucrose fatty acid ester components from A. membranaceus. The nuclear factor-κB (NF-κB) inhibitory activity of isolated compounds was measured in HepG2 cells stimulated with TNF-α using a luciferase reporter system. Among them, compounds 1-6 exhibited significant inhibition of NF-κB activation in a dose-dependent manner, with IC50 values ranging from 4.4 to 24.7 μM. Compounds 1-6 also exhibited inhibition of TNF-α-induced expression of iNOS and ICAM-1 mRNA and dose-dependent inhibition of iNOS promoter activity, with IC50 values ranging from 3.3 to 5.0 μM. These data demonstrate the potential of sucrose fatty acid esters from A. membranaceus to prevent and treat inflammatory diseases.
authors.affiliation: College of Pharmacy, Chungnam National University , Daejeon 305-764, Korea.
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.forename: Ya Nan
authors.initials: YN
authors.lastname: Sun
authors.forename: Xi Tao
authors.initials: XT
authors.lastname: Yan
authors.forename: Seo Young
authors.initials: SY
authors.lastname: Yang
authors.forename: Seok Bean
authors.initials: SB
authors.lastname: Song
authors.forename: Young Mi
authors.initials: YM
authors.lastname: Lee
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology; D027885:Astragalus propinquus / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D004952:Esters / Q000737:chemistry / Q000494:pharmacology*; D056945:Hep G2 Cells / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D018799:Intercellular Adhesion Molecule-1 / Q000235:genetics; D008041:Linoleic Acids / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D016328:NF-kappa B / Q000037:antagonists & inhibitors*; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors / Q000235:genetics; D013395:Sucrose / Q000737:chemistry / Q000494:pharmacology*; D014409:Tumor Necrosis Factor-alpha / Q000494:pharmacology
chemical_list: C000589229:6'-O-linoleyl sucrose; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004952:Esters; D008041:Linoleic Acids; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha; D018799:Intercellular Adhesion Molecule-1; D013395:Sucrose; C496319:NOS2 protein, human; D052247:Nitric Oxide Synthase Type II